公开(公告)号：EP3241823B1

公开(公告)日：2019-04-17

申请号：EP15874912.7

申请日：2015-09-22

申请人： Hitgen Ltd.

发明人： LI, Jin ,  LI, Xueming ,  DOU, Dengfeng ,  WAN, Jinqiao ,  GAO, Jian ,  MU, Yun ,  LI, Caikui ,  PAN, Fei ,  ZHONG, Guoqing ,  HU, Xiao ,  LIU, Shaojun ,  LV, Peng

IPC分类号： C07D401/12 ,  C07D405/12 ,  C07D207/48 ,  A61K31/40 ,  A61P25/00 ,  A61P35/00 ,  A61P37/00

公开(公告)号：EP3241823A1

公开(公告)日：2017-11-08

申请号：EP15874912.7

申请日：2015-09-22

申请人： Hitgen Ltd.

发明人： LI, Jin ,  LI, Xueming ,  DOU, Dengfeng ,  WAN, Jinqiao ,  GAO, Jian ,  MU, Yun ,  LI, Caikui ,  PAN, Fei ,  ZHONG, Guoqing ,  HU, Xiao ,  LIU, Shaojun ,  LV, Peng

IPC分类号： C07D207/48 ,  A61K31/40 ,  A61P25/00 ,  A61P35/00 ,  A61P37/00

CPC分类号： C07D207/48 ,  A61K31/40 ,  C07D401/12 ,  C07D405/12

摘要： The present invention discloses a pyrrolic amide compound shown as a formula I, or crystal forms thereof, and pharmaceutically acceptable salts, hydrates or solvates, wherein R 1 is selected from hydrogen, hydroxyl, cyano, halogen, carboxyl, C 1 -C 6 alkyl and the like; R 2 is selected from hydrogen, hydroxyl, cyano, halogen and the like; R 3 is selected from hydroxyl and the like; X is selected from

group, m is equal to 0, 1, 2 or 3, and n is equal to 0, 1 or 2. The novel compound shown as the formular I provided by the present invention has high deacetylase inhibitory viability; and meanwhile, a method for preparing the novel compound in the present invention has the advantages of fewer steps, simple and convenient operation, safety, environment friendliness, high yield and the like and is very suitable for industrial application.

摘要翻译： 本发明公开了式I所示的吡咯酰胺化合物或其晶型及其药学上可接受的盐，水合物或溶剂化物，其中R 1选自氢，羟基，氰基，卤素，羧基，C 1 -C 6烷基等 ; R2选自氢，羟基，氰基，卤素等; R3选自羟基等; X选自组，m等于0,1,2或3，并且n等于0,1或2.本发明提供的显示为式I的新化合物具有高脱乙酰酶活性抑制活性; 同时本发明的新型化合物的制备方法步骤少，操作简单方便，安全，环保，产率高等优点，非常适合工业应用。